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Assay Detail

CHEMBL1010168

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Binding affinity to human coagulation factor 10a
ChEMBL ↗
61
Total Activities
61
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Coagulation factor X (CHEMBL244) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Highly efficacious factor Xa inhibitors containing alpha-substituted phenylcycloalkyl P4 moieties.
Qiao JX, King SR, He K, Wong PC, Rendina AR, Luettgen JM, Xin B, Knabb RM, Wexler RR, Lam PY.
Bioorg Med Chem Lett (2009) 19 : 462 -468
PubMed 19046881 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 61 9.64 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL540198 — — 1 10.70
CHEMBL456064 — — 1 10.70
CHEMBL456498 — — 1 10.68
CHEMBL461091 — — 1 10.68
CHEMBL471550 — — 1 10.60
CHEMBL446752 — — 1 10.57
CHEMBL461297 — — 1 10.46
CHEMBL460385 — — 1 10.39
CHEMBL456676 — — 1 10.38
CHEMBL518473 — — 1 10.37
CHEMBL518253 — — 1 10.32
CHEMBL461667 — — 1 10.29
CHEMBL453208 — — 1 10.27
CHEMBL468792 — — 1 10.26
CHEMBL464555 — — 1 10.19
CHEMBL471565 — — 1 10.19
CHEMBL465499 — — 1 10.17
CHEMBL457774 — — 1 10.15
CHEMBL445335 — — 1 10.14
CHEMBL451053 — — 1 10.13
CHEMBL231779 APIXABAN 4.0 1 10.10
CHEMBL504703 — — 1 10.10
CHEMBL461453 — — 1 10.08
CHEMBL468782 — — 1 10.07
CHEMBL456677 — — 1 10.03
CHEMBL510030 — — 1 9.96
CHEMBL468783 — — 1 9.92
CHEMBL512288 — — 1 9.85
CHEMBL461454 — — 1 9.85
CHEMBL516771 — — 1 9.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL540198 — Ki = 0.02 nM 10.70
CHEMBL456064 — Ki = 0.02 nM 10.70
CHEMBL461091 — Ki = 0.021 nM 10.68
CHEMBL456498 — Ki = 0.021 nM 10.68
CHEMBL471550 — Ki = 0.025 nM 10.60
CHEMBL446752 — Ki = 0.027 nM 10.57
CHEMBL461297 — Ki = 0.035 nM 10.46
CHEMBL460385 — Ki = 0.041 nM 10.39
CHEMBL456676 — Ki = 0.042 nM 10.38
CHEMBL518473 — Ki = 0.043 nM 10.37
CHEMBL518253 — Ki = 0.048 nM 10.32
CHEMBL461667 — Ki = 0.051 nM 10.29
CHEMBL453208 — Ki = 0.054 nM 10.27
CHEMBL468792 — Ki = 0.055 nM 10.26
CHEMBL471565 — Ki = 0.064 nM 10.19
CHEMBL464555 — Ki = 0.065 nM 10.19
CHEMBL465499 — Ki = 0.068 nM 10.17
CHEMBL457774 — Ki = 0.071 nM 10.15
CHEMBL445335 — Ki = 0.073 nM 10.14
CHEMBL451053 — Ki = 0.074 nM 10.13
CHEMBL231779 APIXABAN Ki = 0.08 nM 10.10
CHEMBL504703 — Ki = 0.079 nM 10.10
CHEMBL461453 — Ki = 0.084 nM 10.08
CHEMBL468782 — Ki = 0.085 nM 10.07
CHEMBL456677 — Ki = 0.093 nM 10.03
CHEMBL510030 — Ki = 0.11 nM 9.96
CHEMBL468783 — Ki = 0.12 nM 9.92
CHEMBL512288 — Ki = 0.14 nM 9.85
CHEMBL461454 — Ki = 0.14 nM 9.85
CHEMBL516771 — Ki = 0.15 nM 9.82
CHEMBL518401 — Ki = 0.16 nM 9.80
CHEMBL516297 — Ki = 0.16 nM 9.80
CHEMBL459286 — Ki = 0.18 nM 9.74
CHEMBL460884 — Ki = 0.18 nM 9.74
CHEMBL206335 RAZAXABAN Ki = 0.19 nM 9.72
CHEMBL465584 — Ki = 0.21 nM 9.68
CHEMBL512467 — Ki = 0.24 nM 9.62
CHEMBL456034 — Ki = 0.24 nM 9.62
CHEMBL512287 — Ki = 0.29 nM 9.54
CHEMBL514567 — Ki = 0.31 nM 9.51
CHEMBL457549 — Ki = 0.32 nM 9.49
CHEMBL464756 — Ki = 0.36 nM 9.44
CHEMBL462710 — Ki = 0.55 nM 9.26
CHEMBL513954 — Ki = 0.56 nM 9.25
CHEMBL467576 — Ki = 0.59 nM 9.23
CHEMBL461668 — Ki = 0.74 nM 9.13
CHEMBL515847 — Ki = 0.78 nM 9.11
CHEMBL515383 — Ki = 1.0 nM 9.00
CHEMBL459102 — Ki = 1.1 nM 8.96
CHEMBL515066 — Ki = 1.1 nM 8.96